U.S. patent application number 10/258814 was filed with the patent office on 2003-09-04 for plant extract of the species <i>vitis vinifera <i> as no-synthase inhibitor and uses.
Invention is credited to Cals-Grieson, Marie-Madeleine.
Application Number | 20030165589 10/258814 |
Document ID | / |
Family ID | 8849753 |
Filed Date | 2003-09-04 |
United States Patent
Application |
20030165589 |
Kind Code |
A1 |
Cals-Grieson,
Marie-Madeleine |
September 4, 2003 |
Plant extract of the species <I>vitis vinifera <I> as
no-synthase inhibitor and uses
Abstract
The invention concerns the use of an efficient amount of at
least an extract of a plant of the species Vitis vinifera in a
physiologically acceptable medium, in a composition or for
preparing a composition, the extract or the composition being
designed to inhibit NO-synthase.
Inventors: |
Cals-Grieson, Marie-Madeleine;
(Meudon, FR) |
Correspondence
Address: |
BURNS DOANE SWECKER & MATHIS L L P
POST OFFICE BOX 1404
ALEXANDRIA
VA
22313-1404
US
|
Family ID: |
8849753 |
Appl. No.: |
10/258814 |
Filed: |
March 26, 2003 |
PCT Filed: |
April 27, 2001 |
PCT NO: |
PCT/FR01/01316 |
Current U.S.
Class: |
424/766 |
Current CPC
Class: |
A61Q 19/004 20130101;
A61P 17/00 20180101; A61Q 5/02 20130101; A61Q 15/00 20130101; A61P
17/14 20180101; A61K 2800/782 20130101; A61Q 19/08 20130101; A61Q
19/005 20130101; A61P 43/00 20180101; A61P 17/16 20180101; A61Q
17/04 20130101; A61Q 19/00 20130101; A61K 8/9789 20170801 |
Class at
Publication: |
424/766 |
International
Class: |
A61K 035/78 |
Foreign Application Data
Date |
Code |
Application Number |
Apr 28, 2000 |
FR |
00/05521 |
Claims
1. The use of an effective amount of at least one extract of at
least one plant of the species Vitis vinifera, in a physiologically
acceptable medium, in a composition or for preparing a composition,
the extract or the composition being intended to inhibit
NO-synthase.
2. The use as claimed in the preceding claim, characterized in that
the extract or the composition is intended to slow down or even
inhibit cellular differentiation and/or proliferation.
3. The use as claimed in the preceding claim, characterized in that
the extract or the composition is intended to slow down or even
inhibit growth of the epidermis and/or to treat hyperproliferative
disorders.
4. The use as claimed in claim 1, characterized in that the extract
or the composition is intended to inhibit degradation and/or
destruction of cells.
5. The use as claimed in claim 1, characterized in that the extract
or the composition is intended to inhibit cellular apoptotic
processes.
6. The use as claimed in claim 1, characterized in that the extract
or the composition is intended to treat intrinsic and/or extrinsic
aging.
7. The use as claimed in claim 1, characterized in that the extract
or the composition is intended to inhibit or even suppress
immunological and/or inflammatory processes.
8. The use as claimed in claim 7, characterized in that the extract
or the composition is intended to treat contact hypersensitivity
reactions and/or allergic manifestations and/or the immune
response.
9. The use as claimed in claim 7, characterized in that the extract
or the composition is intended to decrease or even inhibit
inflammation of the skin.
10. The use as claimed in claim 9, characterized in that the
extract or the composition is intended to treat neurogenic
inflammatory processes of the skin.
11. The use as claimed in claim 1, characterized in that the
extract or the composition is intended to treat "sensitive"
skin.
12. The use as claimed in claim 1, characterized in that the
extract or the composition is intended to treat erythemas,
particularly erythemas induced by ultraviolet radiation.
13. The use as claimed in claim 1, characterized in that the
extract or the composition is intended to treat localized or
diffuse erythematous eruptions of the skin.
14. The use as claimed in claim 1, characterized in that the
extract or the composition is intended to treat acne rosacea.
15. The use as claimed in claim 1, characterized in that the
extract or the composition is intended to inhibit melanogenesis
induced by ultraviolet radiation type A and/or B, and/or to treat
disorders of the hypermelanosis type.
16. The use as claimed in claim 1, characterized in that the
extract or the composition is intended to control sweating.
17. The use as claimed in claim 1, characterized in that the
extract or the composition is intended to stimulate lipolysis.
18. The use as claimed in claim 1, characterized in that the
extract or the composition is intended to inhibit hair loss.
19. The use as claimed in claim 1, characterized in that the
extract or the composition is intended to reinforce the barrier
function of the skin.
20. The use as claimed in claim 1, characterized in that the
extract or the composition is intended to stimulate moisturization
of the skin.
21. The use as claimed in any one of the preceding claims,
characterized in that the extract is in an amount representing from
10.sup.-4% to 20% of the total weight of the composition.
22. The use as claimed in the preceding claim, characterized in
that the extract is in an amount representing from
5.times.10.sup.-3% to 10% of the total weight of the
composition.
23. The use as claimed in any one of the preceding claims,
characterized in that the extract is obtained from plant material
derived from a whole plant or from leaves, from stems, from
flowers, from petals, from seeds or from roots, or else from
dedifferentiated cells.
24. The use as claimed in the preceding claim, characterized in
that the extract is obtained from leaves.
25. The use as claimed in any one of the preceding claims,
characterized in that the extract is obtained from plant material
derived from at least one plant cultured in vivo.
26. A method of cosmetic treatment for the purpose of treating
disorders related to NO synthesis, characterized in that a cosmetic
composition comprising at least one extract of at least one plant
of the species Vitis vinifera, in a physiologically acceptable
medium, is used by application to the skin, to the hair and/or to
the mucous membranes.
Description
[0001] The present invention relates to the use of an effective
amount of at least one extract of at least one plant of the species
Vitis vinifera, in a physiologically acceptable medium, in a
composition or for preparing a composition, the extract or the
composition being intended to inhibit NO-synthase.
[0002] The term "NO-synthase" covers a family of enzymes which
carry out the enzymatic catalysis of L-arginine to citrulline,
during which catalysis a gaseous medium with multiple functions,
nitric oxide, or NO, is produced.
[0003] NO-synthases exist in three forms, two constitutive forms,
nomenclature including neuronal NO-synthase (or NOS 1) and
endothelial NO-synthase (or NOS 3), and the inducible form (or NOS
2) (Medecine/Sciences, 1992, 8, pp. 843-845). It is understood
elsewhere in the text that, unless otherwise indicated, the term
"NO-synthase" covers all the isoforms of the enzyme.
[0004] Thus, according to the invention, the term, "NO-synthase
inhibitors" is intended to mean any product which, ultimately,
notwithstanding the NO-synthase isoform, leads to a decrease in the
concentration of NO. Mention may be made, by way of example, of
products which reduce the amount of active NO-synthase, which block
the enzymatic activity of NO-synthase or its induction, or which
inhibit the activity of the NO produced.
[0005] By virtue of its structure, nitric oxide has an additional
electron which makes it extremely chemically reactive. It is of
note that such compounds are harmful, and the intention is to limit
the production thereof as much as possible. Thus, in the case of
nitric oxide, NO-synthase inhibitors have been widely studied.
[0006] NO is a multifunctional signal molecule which is active in a
large variety of systems and of tissues of the body. Besides its
damaging effects for cells, which are linked to its hyperreactivity
due to its structure comprising an additional electron, it is
acknowledged, inter alia, as being particularly involved in the
cardiovascular system (regulator of blood pressure with vasodilator
effect, inhibitor of platelet aggregation with anticlotting
effect), in the nervous system (memory, modulation of
neurotransmitter release), and in the immune system (modulation of
immune defenses, inflammation, involvement in autoimmune
pathological conditions).
[0007] It is now well accepted that NO plays a predominant role in
the skin. NO can be synthesized by all the varieties of cells which
make up the skin and, therefore, it is involved in multiple and
complex processes of regulation, such as regulation of cellular
differentiation and/or proliferation, of vasodilation, of
melanogenesis, or of the response to environmental variations
(homeostasis).
[0008] Its involvement in cellular differentiation and
proliferation (stimulatory effect), particularly of keratinocytes,
associates it both with growth of the epidermis and cicatrization
and with hyperproliferative disorders (psoriasis).
[0009] Due to its electron hyperreactivity possibly leading to
degradation, or even destruction, of cells, NO is involved in
apoptotic processes and in intrinsic and/or extrinsic aging of the
skin.
[0010] It is involved in immunological and inflammatory processes
of the skin. It is in fact commonly accepted that NO plays a role
in contact hypersensitivity reactions, in allergic manifestations
of the skin, and in the immune response of the skin. Similarly,
besides its direct pro-inflammatory role, it is the mediator
between neuropeptides such as substance P and/or the calcitonin
gene-related peptide (CGRP) in neurogenic inflammatory processes of
the skin, hence its involvement in the phenomena of "sensitive"
skin.
[0011] The involvement of NO in vasodilation means that it is
associated with erythemas of the skin, particularly erythemas
induced by ultraviolet radiation, localized or diffuse erythematous
eruptions of the skin, such as those caused by drugs, toxins and/or
viral or bacterial infections, and with acne rosacea.
[0012] NO is acknowledged to be an intermediate in the
melanogenesis induced by ultraviolet radiation type B (UVB). It is
also thought to be one of the factors involved in disorders of the
hypermelanosis type.
[0013] NO also appears to be involved in the control of sweating
and also in that of lipolysis (inhibitory effect), or in hair
loss.
[0014] Finally, NO is known to have an influence on the barrier
function of the skin and therefore on the moisturization thereof
(inhibitory effect).
[0015] The advantage which exists in having NO-synthase inhibitors
can therefore be understood.
[0016] In this regard, many inhibitors have already been proposed
in the prior art. Mention may be made more particularly of
N.sup.G-monomethyl-L-arginine (NMMA), N.sup.G-nitro-L-arginine
methyl ester (NAME), N.sup.G-nitro-L-arginine (NNA),
N.sup.G-amino-L-arginine (NAA), N.sup.G,N.sup.G-dimethylarginine
(asymmetric dimethylarginine, called ADMA), diphenyleneiodonium
chloride, 2-(4-carboxyphenyl)-4,4,5,5-t-
etramethylimidazoline-1-oxy 3-oxide, 7-nitroindazole,
N(5)-(1-iminoethyl)-L-ornithine, aminoguanidine, canavanine and
ebselen.
[0017] Without casting doubt on the effectiveness of these
products, it is noted that they are chemical compounds which may
induce problems, or even harmful side effects, in users, who
generally prefer using natural products.
[0018] The aim of the present invention is to provide a novel
NO-synthase inhibitor which is also a natural NO-synthase
inhibitor.
[0019] Surprisingly and unexpectedly, the applicant has
demonstrated that at least one extract of at least one plant of the
species Vitis vinifera has the property of being an NO-synthase
inhibitor, particularly an inhibitor of inducible NO synthase (NOS
2), which makes it a good candidate for uses in applications in
which it proves to be advantageous to use an NO-synthase inhibitor,
particularly in cosmetics.
[0020] Extracts of a plant of the species Vitis vinifera are known,
in the prior art, to promote vasodilation or else in that they can
be used in compositions intended for skin care and/or hair
care.
[0021] However, to the applicant's knowledge, it has never been
described that an extract of at least one plant of the species
Vitis vinifera has the property of being an NO-synthase inhibitor,
particularly an inducible NO-synthase (NOS 2) inhibitor.
[0022] The first subject of the invention is therefore the use of
an effective amount of at least one extract of at least one plant
of the species Vitis vinifera, in a physiologically acceptable
medium, in a composition or for preparing a composition, the
extract or the composition being intended to inhibit NO-synthase,
particularly inducible NO-synthase (NOS 2).
[0023] The expression "physiologically acceptable medium" is
understood to mean a medium compatible with the skin, the mucous
membranes, the nails and the hair.
[0024] The second subject of the invention is the use of an
effective amount of at least one extract of at least one plant of
the species Vitis vinifera, in a physiologically acceptable medium,
in a composition or for preparing a composition, the extract or the
composition being intended for use in all domains in which
inhibition of NO-synthases, particularly of inducible NO-synthase
(NOS 2), proves to be necessary, particularly in the domain of the
skin and/or of the hair.
[0025] Thus, the extract of a plant of the species Vitis vinifera
or the composition containing it, may be used to slow down or even
inhibit cellular differentiation and/or proliferation, and/or
vasodilation, and/or melanogenesis, and/or the response to
environmental variations (homeostasis).
[0026] Thus, the third subject of the invention is the use of an
effective amount of at least one extract of at least one plant of
the species Vitis vinifera, in a physiologically acceptable medium,
in a composition or for preparing a composition, the extract or the
composition being intended to slow down or even inhibit cellular
differentiation and/or proliferation, particularly to regulate
growth of the epidermis and/or to treat hyperproliferative
disorders such as, for example, psoriasis.
[0027] The fourth subject of the invention is the use of an
effective amount of at least one extract of at least one plant of
the species Vitis vinifera, in a. physiologically acceptable
medium, in a composition or for preparing a composition, the
extract or the composition being intended to inhibit degradation
and/or destruction of cells and to inhibit apoptotic processes,
particularly of skin cells, very particularly of keratinocytes,
and/or to treat intrinsic and/or extrinsic aging of cells,
particularly of skin cells.
[0028] The fifth subject of the invention is the use of an
effective amount of at least one extract of at least one plant of
the species Vitis vinifera, in a physiologically acceptable medium,
in a composition or for preparing a composition, the extract or the
composition being intended to inhibit or even suppress the
immunological and/or inflammatory processes related to NO
synthesis, such as for example contact hypersensitivity reactions
and/or allergic manifestations and/or the immune response,
particularly of the skin.
[0029] The extract or the composition is particularly intended to
decrease or even inhibit inflammation of the skin, very
particularly neurogenic inflammatory processes of the skin, and
therefore to treat "sensitive" skin.
[0030] The sixth subject of the invention is the use of an
effective amount of at least one extract of at least one plant of
the species Vitis vinifera, in a physiologically acceptable medium,
in a composition or for preparing a composition, the extract or the
composition being intended to treat acne rosacea and/or erythemas
of the skin, particularly erythemas induced by ultraviolet
radiation and/or localized or diffuse erythematous eruptions of the
skin, such as those caused by drugs, toxins and/or viral or
bacterial infections.
[0031] The seventh subject of the invention is the use of an
effective amount of at least one extract of at least one plant of
the species Vitis vinifera, in a physiologically acceptable medium,
in a composition or for preparing a composition, the extract or the
composition being intended to inhibit melanogenesis induced by
ultraviolet radiation type A and/or B, and/or to treat disorders of
the hypermelanosis type.
[0032] The eighth subject of the invention is the use of an
effective amount of at least one extract of at least one plant of
the species Vitis vinifera, in a physiologically acceptable medium,
in a composition or for preparing a composition, the extract or the
composition being intended to control sweating and/or to stimulate
lipolysis and/or to inhibit hair loss and/or to reinforce the
barrier function of the skin and/or to stimulate moisturization of
the skin.
[0033] According to the invention, the composition comprising the
extract may be a cosmetic or dermatological composition.
Preferentially according to the invention, the composition is a
cosmetic composition.
[0034] Preferentially according to the invention, the extract or
the composition comprising it is applied to the skin topically.
[0035] The plant of the species Vitis vinifera is one of the 28
plant species belonging to the genus Vitis which, itself, belongs
to the family Ampelideae.
[0036] Of course, the extract may be prepared from at least any one
of the many varieties associated with each of the plant species
belonging to the genus Vitis. It is therefore understood that, in
the text, the term "Vitis vinifera" should be taken to denote any
one of the many plant varieties associated with each of the plant
species belonging to the genus Vitis, and particularly to denote
the species Vitis vinifera.
[0037] The extract of a plant of the species Vitis vinifera may be
any extract prepared from any plant material derived from at least
one plant of the genus Vitis.
[0038] Thus, [lacuna] of a plant of the species Vitis vinifera used
according to the invention may be obtained from plant material
derived from a whole plant or from parts of a plant, such as the
leaves, the stems, the flowers, the petals, the seeds or the roots,
or else dedifferentiated cells.
[0039] The term "dedifferentiated plant cells" is intended to mean
any plant cell which shows none of the characteristics of a
particular specialization and which is capable of living by itself
and not in a state of dependency with other cells.
[0040] Preferentially according to the invention, an extract
prepared from green leaves is used.
[0041] The extract of at least one plant of the genus Vitis may be
any extract prepared from any plant material derived from at least
one plant of the genus Vitis, cultured in vivo or derived from
culturing in vitro.
[0042] The term "culturing in vivo" is intended to mean any
culturing of the conventional type, i.e. in soil in the open air or
under glass, or else out of soil.
[0043] The term "culturing in vitro" is intended to mean all of the
techniques known to those skilled in the art which make it possible
to artificially obtain a plant or a part of a plant. The selection
pressure imposed by the physicochemical conditions during growth of
the plant cells in vitro makes it possible to obtain a standardized
plant material which is available throughout the year, unlike the
plants cultured in vivo.
[0044] Preferentially according to the invention, a plant derived
from culturing in vivo is used.
[0045] Any extraction method known to those skilled in the art may
be used to prepare the extract contained in the composition
according to the invention.
[0046] Mention may in particular be made of aqueous or alcoholic
extracts or extracts using an organic solvent.
[0047] The term "aqueous solvent" is intended to mean any solvent
consisting totally or partly of water. Mention may thus be made of
water itself, aqueous-alcoholic solvents in any proportion or
solvents consisting of water and a compound such as propylene
glycol in any proportion.
[0048] Among the alcoholic solvents, mention may in particular be
made of ethanol.
[0049] Use may also be made of an extract prepared using the method
described in French patent application No. 95-02379 filed by the
applicant. Thus, in a first step, the plant material is ground in
an aqueous solution under cold conditions, in a second step, the
particles in suspension are removed from the aqueous solution
derived from the first step and, in a third step, the aqueous
solution derived from the second step is sterilized. This aqueous
solution corresponds to the extract.
[0050] Furthermore, the first step may advantageously be replaced
with an operation of simply freezing the plant tissues (for example
at -20.degree. C.), followed by aqueous extraction repeating the
second and third steps described above.
[0051] Whatever the preparation mode used according to the
invention, subsequent steps aimed at promoting conservation and/or
stabilization may be added without, for all that, modifying the
very nature of the extract. Thus, for example, the extract obtained
may be lyophilized using any conventional lyophilization methods. A
powder is thus obtained, which may be used directly or else mixed
in a suitable solvent before use.
[0052] Mention may also be made of commercial extracts such as that
sold by the company Euromed under the name "Leucocyanidines de
raisins extra" [grape Leucocyanidin extra], or else that sold by
the company Indena under the name Leucoselecta or, finally, that
sold by the company Hansen under the name "extrait de marc de
raisin" [grape marc extract].
[0053] Preferentially according to the invention, an extract sold
by the company Euromed under the name "Leucocyanidines de raisins
extra" [grape Leucocyanidin extra] is used.
[0054] According to the invention, the amount of extract of a plant
of the species Vitis vinifera used in the composition depends, of
course, on the desired effect and may therefore vary within a wide
range.
[0055] To give an order of magnitude, according to the invention,
the extract may be used in an amount representing from 10.sup.-4%
to 20% of the total weight of the composition, and preferentially
in an amount representing from 5.times.10.sup.-3% to 10%, of the
total weight of the composition.
[0056] Of course, according to the invention, the extract of at
least one plant of the species Vitis vinifera may be combined with
other NO-synthase inhibitors, for instance lipochroman-6, for
example, or other plant extracts, such as, for example, an extract
of Ginkgo biloba, an extract of Olea europaea or an extract of
green tea or of cacao.
[0057] The ninth subject of the invention is a method of cosmetic
treatment for the purpose of treating disorders related to NO
synthesis, characterized in that a cosmetic composition comprising
at least one extract of at least one plant of the species Vitis
vinifera, in a physiologically acceptable medium, is used by
application to the skin, to the hair and/or to the mucous
membranes.
[0058] The method of cosmetic treatment of the invention is aimed
at improving the appearance of the individual suffering from
disorders due to NO synthesis.
[0059] The method of cosmetic treatment of the invention may in
particular be used by applying the cosmetic compositions as defined
above, according to the normal technique for using these
composition. Thus, for example, it is possible to apply creams,
gels, sera, lotions, make-up-removing milks or antisun compositions
to the skin or to dry hair, to apply a hair lotion to wet hair or
to apply shampoos, or to apply dentifrice to the gums.
[0060] Whatever the form of the composition according to the
invention in which the extract is used, it may be ingested,
injected or applied to the skin (to any area of body skin), the
hair, the nails or the mucous membranes (oral, jugal, gingival,
genital or. conjunctival membranes). Depending on the method of
administration, the composition according to the invention may be
in any pharmaceutical form normally used.
[0061] For a topical application to the skin, the composition may
in particular be in the form of an aqueous or oily solution or of a
dispersion of the lotion or serum type, of emulsions of liquid or
semi-liquid consistency of the milk type, obtained by dispersing a
fatty phase in an aqueous phase (O/W emulsion) or conversely (W/O
emulsion), or of suspensions or emulsions of soft consistency of
the aqueous or anhydrous cream or gel type, or alternatively of
microcapsules or microparticles, or of vesicular dispersions of
ionic and/or nonionic type. These compositions are prepared
according to the usual methods.
[0062] They may also be used for the hair in the form of aqueous,
alcoholic or aqueous-alcoholic solutions, or in the form of creams,
of gels, of emulsions or of foams, or alternatively in the form of
aerosol compositions also comprising a pressurized propellant.
[0063] For injection, the composition may be in the form of an
aqueous or oily lotion or in the form of serum. For the eyes, it
may be in the form of drops and, for ingestion, it may be in the
form of capsules, of granules, of syrups or of tablets.
[0064] The amounts of the various constituents of the compositions
according to the invention are those conventionally used in the
domains under consideration.
[0065] These compositions in particular constitute cleansing,
protective, treating or care creams for the face, for the hands,
for the feet, for the major anatomical folds or for the body (for
example day creams, night creams, make-up removing creams,
foundation creams and antisun creams), fluid foundations,
make-up-removing milks, protective body milks or bodycare milks,
antisun milks, skincare lotions, gels or mousses, for instance
cleansing lotions, antisun lotions, artificial tanning lotions,
bath compositions, deodorant compositions comprising a bactericidal
agent, aftershave gels or lotions, hair-removing creams,
insect-repellent compositions, pain-relief compositions,
compositions for treating certain diseases of the skin, such as
eczema, acne rosacea, psoriasis, lichens and severe pruritis.
[0066] The compositions according to the invention may also consist
of solid preparations constituting cleansing soaps or bars.
[0067] The compositions may also be packaged in the form of an
aerosol composition also comprising a pressurized propellant.
[0068] The composition according to the invention may also be a
haircare composition, and especially a shampoo, a setting lotion, a
treating lotion, a styling cream or gel, a dye composition
(especially for oxidation dyeing) optionally in the form of
coloring shampoos, restructuring lotions for the hair, a
permanent-waving composition (in particular a composition for the
first stage of a permanent-waving operation), a lotion or a gel for
preventing hair loss, an antiparasitic shampoo, etc.
[0069] The composition may also be for orodental use, for example a
toothpaste. In this case, the composition may contain adjuvants and
additives which are usual for compositions for oral use and, in
particular, surfactants, thickeners, wetting agents, polishing
agents such as silica, various active ingredients such as
fluorides, in particular sodium fluoride, and optionally sweeteners
such as sodium saccharinate.
[0070] When the composition is an emulsion, the proportion of the
fatty phase may range from 5% to 80% by weight, and preferably from
5% to 5.0% by weight, relative to the total weight of the
composition. The oils, waxes, emulsifiers and co-emulsifiers used
in the composition in emulsion form are chosen from those
conventionally used in cosmetics. The emulsifier and co-emulsifier
are present, in the composition, in an amount ranging from 0.3% to
30% by weight, and preferably from 0.5 to 20% by weight, relative
to the total weight of the composition. The emulsion may also
contain lipid vesicles.
[0071] When the composition is an oily solution or gel, the fatty
phase may represent more than 90% of the total weight of the
composition.
[0072] In a known manner, the cosmetic composition may also contain
adjuvants that are common in cosmetics, such as hydrophilic or
lipophilic gelling agents, hydrophilic or lipophilic additives,
preserving agents, antioxidants, solvents, fragrances, fillers,
screening agents, odor absorbers and dyestuffs. The amounts of
these various adjuvants are those conventionally used in cosmetics
and, for example, from 0.01% to 10% of the total weight of the
composition. Depending on their nature, these adjuvants may be
introduced into the fatty phase, into the aqueous phase and/or into
the lipid spherules.
[0073] As oils or waxes which may be used in the invention, mention
may be made of mineral oils (liquid petroleum jelly), plant oils
(liquid fraction of karite butter or sunflower oil), animal oils
(perhydrosqualene), synthetic oils (Purcellin oil), silicone oils
or waxes (cyclomethicone) and fluoro oils (perfluoropolyethers),
beeswax, carnauba wax or paraffin wax. Fatty alcohols or fatty
acids (stearic acid) may be added to these oils.
[0074] As emulsifiers which may be used in the invention, mention
may be made, for example, of glyceryl stearate, polysorbate 60 and
the mixture of PEG-6/PEG-32/glycol stearate sold under the name
Tefose.sup.R 63 by the company Gattefosse.
[0075] As solvents which may be used in the invention, mention may
be made of lower alcohols, in particular ethanol and isopropanol,
and propylene glycol.
[0076] As hydrophilic gelling agents which may be used in the
invention, mention may be made of carboxyvinyl polymers (carbomer),
acrylic copolymers such as acrylate/alkyl acrylate copolymers,
polyacrylamides, polysaccharides such as hydroxypropylcellulose,
natural gums and clays, and, as lipophilic gelling agents, mention
may be made of modified clays, such as bentones, metal salts of
fatty acids, such as aluminum stearates, and hydrophobic silica,
ethylcellulose and polyethylene.
[0077] The composition may contain other hydrophilic active agents,
such as proteins or protein hydrolyzates, amino acids, polyols,
urea, allantoin, sugars and sugar derivatives, water-soluble
vitamins, plant extracts and hydroxy acids.
[0078] Lipophilic active agents which may be used include retinol
(vitamin A) and derivatives thereof, tocopherol (vitamin E) and
derivatives thereof, essential fatty acids, ceramides, essential
oils, and salicylic acid and derivatives thereof.
[0079] According to the invention, the composition may combine at
least one extract of at least one plant of the species Vitis
vinifera with other active agents in particular intended to prevent
and/or treat skin ailments. Among these active agents, mention may
be made, by way of example, of:
[0080] agents for modifying differentiation and/or proliferation
and/or pigmentation of the skin, such as retinoic acid and isomers
thereof, retinol and esters thereof, vitamin D and derivatives
thereof, kojic acid or hydroquinone;
[0081] antibacterial agents, such as clindamycin phosphate or
erythromycin or antibiotics of the tetracyclin family;
[0082] antiparasitic agents, in particular metronidazole,
crotamiton or pyrethrinoids;
[0083] antifungal agents, in particular compounds belonging to the
imidazole family, such as econazole, ketoconazole or miconazole, or
salts thereof, polyene compounds, such as amphotericin B, compounds
of the allylamine family, such as terbinafine, or alternatively
octopirox;
[0084] nonsteroidal antiinflammatory agents, such as ibuprofen and
salts thereof, diclofenac and salts thereof, acetylsalicylic acid,
acetaminophen or glycyrrhetinic acid;
[0085] anesthetics, such as lidocaine hydrochloride and derivatives
thereof;
[0086] antipruriginous agents, such as thenaldine, trimeprazine or
cyproheptadine;
[0087] keratolytic agents, such as alpha- and
beta-hydroxycarboxylic acids or beta-keto carboxylic acids, their
salts, amides or esters and more particularly hydroxy acids such as
glycolic acid, lactic acid, salicylic acid, citric acid and fruit
acids in general, and 5-n-octanoylsalicylic acid;
[0088] free-radical scavengers, such a alpha-tocopherol or esters
thereof, superoxide dismutases, certain metal chelating agents, or
ascorbic acid and esters thereof;
[0089] antiseborrheic agents, such as progesterone;
[0090] antidandruff agents, such as octopirox or zinc
pyrithione;
[0091] antiacne agents, such as retinoic acid or benzoyl
peroxide;
[0092] plant extracts or extracts of microbial origin;
[0093] peptides and derivatives thereof, such as, for example, the
tripeptide Lys-Pro-Val.
[0094] The following examples and compositions illustrate the
invention without in any way limiting it. In the compositions, the
proportions given are percentages by weight.
EXAMPLE 1
[0095] Biological Activity of Commercial Extracts of a Plant of the
Species Vitis vinifera:
[0096] The assay is carried out with three commercial extracts,
namely:
[0097] 1: Extract sold by the company Euromed under the name
"Leucocyanidines de raisins extra" [grape Leucocyanidin extra],
[0098] 2. Extract sold by the company Indena under the name
Leucoselect.RTM.,
[0099] 3. Extract sold by the company Hansen under the name
"extrait de marc de raisin" [grape marc extract].
[0100] The activity of the extracts on inducible NO-synthase was
evaluated in the test described by Heck et al. (J.B.C., Vol. 267,
No. 30, 21277-21280, Oct. 25, 1992).
[0101] The aim of this test is to demonstrate the decrease in
nitrate and nitrite concentration, ultimately, after stimulation of
NO-synthase 2.
[0102] A: positive control (induction of the enzyme): mixtures of
.gamma.-interferon (1 000 U/ml) and interleukin-1.beta. (100
U/ml);
[0103] B: negative control (maximum inhibition):
N.sup.G-monomethyl-L-argi- nine (L form) at 200 .mu.M;
[0104] C: control for specificity of inhibition:
N.sup.G-monomethyl-L-argi- nine (D form) at 200 .mu.M.
[0105] In order to determine the activity of the product to be
tested, the amount of stable NO reaction products (nitrites and
nitrates) is measured using the nitric calorimetric assay kit sold
by the company Boehringer under the reference 1756.28.
[0106] Each extract was tested at the concentrations of 0.001%,
0.005% and 0.01% (weight/volume).
1 Product % tested inhibition A 0 B 100 C 0 1 0.001% 20 0.005% 50
0.01% 68 2 0.001% 20 0.005% 30 0.01% 53 3 0.001% 15 0.005% 30 0.01%
49
[0107] The extracts have an inhibitory effect on inducible
NO-synthase.
EXAMPLE 2
[0108] Examples of formulations illustrating the invention. These
compositions were obtained by simply mixing the various
components.
2 Composition 1: Lotion Extract 1 2.00% Antioxidant 0.05%
Isopropanol 40.00% Preserving agent 0.30% Water qs for 100%
Composition 2: Care gel Extract 2 3.00% Hydroxypropylcellulose*
1.00% Antioxidant 0.05% Isopropanol 40.00% Preserving agent 0.30%
Water qs for 100% Composition 3: Care cream (oil-in-water emulsion)
Extract 3 5.00% Glyceryl stearate 2.00% Polysorbate 60** 1.00%
Stearic acid 1.40% Triethanolamine 0.70% Carbomer 0.40% Liquid
fraction of karite butter 12.00% Perhydrosqualene 12.00%
Antioxidant 0.05% Fragrance 0.50% Preserving agent 0.30% Water qs
for 100% Composition 4: Shampoo Extract 3 0.50%
Hydroxypropylcellulose* 1.00% Fragrance 0.50% Preserving agent
0.30% Water qs for 100% Composition 5: Care cream (oil/water
emulsion) Extract 1 5.00% Glyceryl stearate 2.00% Polysorbate 60**
1.00% Stearic acid 1.40% 5-n-octanoylsalicylic acid 0.50%
Triethanolamine 0.70% Carbomer 0.40% Liquid fraction of karite
butter 12.00% Perhydrosqualene 12.00% Antioxidant 0.05% Fragrance
0.50% Preserving agent 0.30% Water qs for 100% Composition 6:
Pain-relieving gel Extract 2 5.00% Hydroxypropylcellulose* 1.00%
Antioxidant 0.05% Lidocaine hydrochloride 2.00% Isopropanol 40.00%
Preserving agent 0.30% Water qs for 100% Composition 7: Care cream
for sunburn (oil-in-water emulsion) Extract 1 5.00% Glyceryl
stearate 2.00% Polysorbate 60** 1.00% Stearic acid 1.40%
Glycyrrhetinic acid 2.00% Triethanolamine 0.70% Carbomer 0.40%
Liquid fraction of karite butter 12.00% Sunflower oil 10.00%
Antioxidant 0.05% Fragrance 0.50% Preserving agent 0.30% Water qs
for 100% Composition 8: Gel for treating acne Extract 3 5.00%
All-trans retinoic acid 0.05 Hydroxypropylcellulose* 1.00%
Antioxidant 0.05% Isopropanol 40.00% Preserving agent 0.30% Water
qs for 100% Composition 9: Lotion for eliminating scars due to acne
Extract 2 3.00% Glycolic acid 50.00% Hydroxypropylcellulose* 0.05%
Preserving agent 0.30% NaOH qs for pH = 2.8% Ethanol qs for 100% *:
Klucel H .RTM. sold by the company Hercules **: Tween 60 .RTM. sold
by the company ICI
* * * * *